| Bioactivity | Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. | ||||||||||||
| Target | Ki: 0.7 nM (CB1) | ||||||||||||
| Invitro | Otenabant HCl has low affinity with Ki of 7.6 μM for human CB2 receptors[1]. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration[2]. | ||||||||||||
| In Vivo | Otenabant acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. Otenabant (10 mg/kg, p.o.) promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice[1]. Otenabant HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. Otenabant HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation[2]. | ||||||||||||
| Name | Otenabant | ||||||||||||
| CAS | 686344-29-6 | ||||||||||||
| Formula | C25H25Cl2N7O | ||||||||||||
| Molar Mass | 510.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. John R. Hadcock, et al. In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB1 receptor antagonist for the management of obesity. Biochemical and Biophysical Research Communications, 2010; 394;366-371. [2]. Griffith DA, et al. Discovery of 1-[9-(4-chlorophenyl) -8-(2-chlorophenyl)- 9H-purin-6-yl] -4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. JMedChem. 2009 ;5 |
Otenabant
CAS: 686344-29-6 F: C25H25Cl2N7O W: 510.42
Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater
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